Efficient and Site-Specific ¹²⁵I-Radioiodination of Bioactive Molecules Using Oxidative Condensation Reaction.

ABSTRACT: In this report, the novel and site-specific radioiodination of biomolecules by using aryl diamine and alkyl aldehyde condensation reaction in the presence of a Cu²⁺ catalyst under ambient conditions was reported. ¹²⁵I-labeled alkyl aldehyde was synthesized using a tin precursor with a high radiochemical yield (72 ± 6%, n = 5) and radiochemical purity (>99%). The utility of the radioiodinated precursor was demonstrated through aryl diamine-installed c[RGDfK(C)] peptide and human serum albumin (HSA). Radioiodinated c[RGDfK(C)] peptide and HSA protein were synthesized with high radiochemical yields and purity. ¹²⁵I-HSA protein showed excellent in vivo stability and negligible thyroid uptake as compared with directly radioiodinated HSA by using th

SUBMITTER: Mushtaq S 

PROVIDER: S-EPMC6044831 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature